Beer M S, Stanton J A, Bevan Y, Chauhan N S, Middlemiss D N
Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, U.K.
Eur J Pharmacol. 1992 Mar 24;213(2):193-7. doi: 10.1016/0014-2999(92)90681-s.
The ability of three 5-HT1 receptor agonists, 5-HT (5-hydroxytryptamine), 5-CT (5-carboxyamidotryptamine) and sumatriptan to inhibit the binding of [3H]5-HT, in the presence of cyanopindolol and mesulergine, from cerebral cortical and/or caudate membranes in seven species (dog, guinea-pig, rabbit, pig, human, hamster and calf) has been investigated. Under the experimental conditions used, 5-CT and sumatriptan consistently yielded displacement curves best fit to a two-site model whereas 5-HT always gave a monophasic displacement curve. The pIC50 values obtained with 5-HT displacement gave a mean of 8.1 +/- 0.1 (mean +/- S.E.M.). In contrast the biphasic displacement curves for 5-CT and sumatriptan yielded high and low affinity pIC50 values of 8.3 +/- 0.1, 5.5 +/- 0.1 and 7.6 +/- 0.1, 5.0 +/- 0.1, respectively. These data indicate that under these experimental conditions the high affinity component labelled by [3H]5-HT is the same receptor subtype, previously denoted the 5-HT1D receptor, in all seven species.
研究了三种5-羟色胺1（5-HT1）受体激动剂，即5-羟色胺（5-HT，5-hydroxytryptamine）、5-羧基酰胺色胺（5-CT，5-carboxyamidotryptamine）和舒马曲坦，在氰吲哚洛尔和甲磺麦角林存在的情况下，对七种动物（狗、豚鼠、兔子、猪、人、仓鼠和小牛）大脑皮质和/或尾状核膜中[3H]5-HT结合的抑制能力。在所采用的实验条件下，5-CT和舒马曲坦始终产生最符合双位点模型的置换曲线，而5-HT始终给出单相置换曲线。5-HT置换得到的pIC50值平均为8.1±0.1（平均值±标准误）。相比之下，5-CT和舒马曲坦的双相置换曲线分别产生高亲和力和低亲和力的pIC50值，分别为8.3±0.1、5.5±0.1和7.6±0.1、5.0±0.1。这些数据表明，在这些实验条件下，[3H]5-HT标记的高亲和力成分在所有七种动物中都是相同的受体亚型，即先前命名的5-HT1D受体。
